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Chinese scholars have developed a new Zanamivir molecule, drug-resistant influenza virus will be overcome

2016-10-19 来源:转载自第三方
10 October 2016

  Recently, the Institute of Microbiology, Chinese Academy of Sciences, Gao Fu Research Group and Li Xuebing research group developed a new compound with high anti-influenza activity TZ12. The study was published in the journal “Journal of Medicinal Chemistry”, entitled "Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses" [1].
  Influenza is zoonotic respiratory diseases caused by influenza virus, influenza virus has the advantages of fast mutation, high transmission and more harmful. Zanamivir and Tamiflu are common anti-influenza drugs, but the mutant drug-resistant virus strain reduces the binding of the drug and does not play a role in inhibiting the virus.
  In this study, researchers use computer-aided drug development technology to develop a series of tetravalent zanamivir molecules, compared with the existing anti-influenza drug zanamivir (zanamivir), the molecular has a more excellent neuraminidase (NA) affinity, inhibitory activity, and in vivo and in vitro antiviral activity, intranasal administration of TZ12 once to mice infected with influenza virus can protect all mice, which has the potential for further preclinical development.
  Compared with the traditional structure of Zanamivir, how does TZ12 play the role? The complex structure of the viral neuraminidase and TZ12 crystal can explain this function: the four zanamivir antiviral groups of TZ12 can simultaneously enter the four active sites on the neuraminidase (NA) tetramer , Thus forming a thermodynamically more stable 1:1 complex with NA tetramers, which explains the reason why TZ12 is highly effective against influenza virus activity from the mechanism of action.
  This study has designed a new type of highly effective anti-influenza drug against drug-resistant strains, which is of great scientific significance and value. The design method described in this study also provides a more reasonable and effective method for drug design based on target protein structure.
[1] Lifeng Fu, Yuhai Bi, Yan Wu, et al. Structure-based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-resistant Influenza Viruses. Journal of Medicinal Chemistry, 2016, doi: 10.1021 / acs.jmedchem.6b00537.
Related links: Zanamivir
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